TWI530288B - （ｅ）－ｎ－［４－［［３－氯－４－（２－吡啶基甲氧基）苯基］胺基］－３－氰基－７－乙氧基－６－喹啉基］－３－［（２ｒ）－１－甲基吡咯烷－２－基］丙－２－烯醯胺的可藥用的鹽、其製備方法及其在醫藥上的應用 - Google Patents

（ｅ）－ｎ－［４－［［３－氯－４－（２－吡啶基甲氧基）苯基］胺基］－３－氰基－７－乙氧基－６－喹啉基］－３－［（２ｒ）－１－甲基吡咯烷－２－基］丙－２－烯醯胺的可藥用的鹽、其製備方法及其在醫藥上的應用 Download PDF

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Publication number
TWI530288B
TWI530288B TW101106172A TW101106172A TWI530288B TW I530288 B TWI530288 B TW I530288B TW 101106172 A TW101106172 A TW 101106172A TW 101106172 A TW101106172 A TW 101106172A TW I530288 B TWI530288 B TW I530288B
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Taiwan
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salt
amino
chloro
methylpyrrolidin
phenyl
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TW101106172A
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English (en)
Chinese (zh)
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TW201236684A (en
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李心
王斌
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上海恆瑞醫藥有限公司
江蘇恆瑞醫藥股份有限公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/145—Maleic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW101106172A 2011-03-11 2012-02-24 （ｅ）－ｎ－［４－［［３－氯－４－（２－吡啶基甲氧基）苯基］胺基］－３－氰基－７－乙氧基－６－喹啉基］－３－［（２ｒ）－１－甲基吡咯烷－２－基］丙－２－烯醯胺的可藥用的鹽、其製備方法及其在醫藥上的應用 TWI530288B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2011100623598A CN102675287A (zh) 2011-03-11 2011-03-11 (e)-n-[4-[[3-氯-4-(2-吡啶基甲氧基)苯基]氨基]-3-氰基-7-乙氧基-6-喹啉基]-3-[(2r)-1-甲基吡咯烷-2-基]丙-2-烯酰胺的可药用的盐、其制备方法及其在医药上的应用

Publications (2)

Publication Number Publication Date
TW201236684A TW201236684A (en) 2012-09-16
TWI530288B true TWI530288B (zh) 2016-04-21

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TW101106172A TWI530288B (zh) 2011-03-11 2012-02-24 （ｅ）－ｎ－［４－［［３－氯－４－（２－吡啶基甲氧基）苯基］胺基］－３－氰基－７－乙氧基－６－喹啉基］－３－［（２ｒ）－１－甲基吡咯烷－２－基］丙－２－烯醯胺的可藥用的鹽、其製備方法及其在醫藥上的應用

Country Status (12)

Country Link
US (1) US20130338190A1 (fr)
EP (1) EP2684877B1 (fr)
JP (1) JP6192544B2 (fr)
KR (1) KR101871889B1 (fr)
CN (2) CN102675287A (fr)
ES (1) ES2605564T3 (fr)
HK (1) HK1177461A1 (fr)
PL (1) PL2684877T3 (fr)
PT (1) PT2684877T (fr)
RU (1) RU2583056C2 (fr)
TW (1) TWI530288B (fr)
WO (1) WO2012122865A2 (fr)

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CN103539783A (zh) * 2012-07-12 2014-01-29 江苏恒瑞医药股份有限公司 一种酪氨酸激酶抑制剂的二马来酸盐的i型结晶及制备方法
US11065241B2 (en) * 2016-01-27 2021-07-20 Jiangsu Hengrui Medicine Co., Ltd. Pharmaceutical composition comprising quinoline derivative or salt thereof
EP3378479B1 (fr) * 2016-01-27 2020-06-17 Jiangsu Hengrui Medicine Co., Ltd. Procédé de préparation d'une composition pharmaceutique comprenant un dérivé de quinoléine ou un sel de celui-ci
CN112426424A (zh) * 2016-01-28 2021-03-02 江苏恒瑞医药股份有限公司 一种egfr/her2受体酪氨酸激酶抑制剂在制备治疗her2突变癌症药物中的用途
TWI739825B (zh) * 2016-04-28 2021-09-21 大陸商江蘇恆瑞醫藥股份有限公司 一種製備酪胺酸激酶抑制劑及其衍生物的方法
CN107638424B (zh) * 2016-07-20 2022-05-27 江苏恒瑞医药股份有限公司 一种egfr/her2受体酪氨酸激酶抑制剂在制备治疗癌症的药物中的用途
EP3572082A4 (fr) * 2017-01-22 2021-01-06 Jiangsu Hengrui Medicine Co., Ltd. Utilisations d'un inhibiteur de egfr/her2 combiné à un médicament anti-métabolique de type pyrimidine
KR20200072491A (ko) * 2017-10-18 2020-06-22 지앙수 헨그루이 메디슨 컴퍼니 리미티드 티로신 키나제 억제제 및 이의 중간체의 제조 방법
KR20200078561A (ko) 2017-10-24 2020-07-01 지앙수 헨그루이 메디슨 컴퍼니 리미티드 퀴놀린 유도체를 함유하는 약학 조성물
US11034656B2 (en) * 2017-11-20 2021-06-15 Teligene Ltd. Maleate salts of (E)-N-(3-cyano-7-ethoxy-4-((4-phenoxyphenyl)amino) quinolin-6-yl)-4-(dimethylamino)but-2-enamide and crystalline forms thereof
US10857146B2 (en) 2018-08-21 2020-12-08 Jiangsu Hengrui Medicine Co., Ltd. Method for preventing or treating tumor diseases with a combination of tyrosine kinase inhibitor and CDK4/6 inhibitor
CN110960529A (zh) * 2018-09-30 2020-04-07 江苏恒瑞医药股份有限公司 一种降低了毒性杂质含量的酪氨酸激酶抑制剂的原料药
WO2020083188A1 (fr) 2018-10-22 2020-04-30 江苏恒瑞医药股份有限公司 Forme cristalline de maléate d'inhibiteur de tyrosine kinase et son procédé de préparation
CN111821304A (zh) * 2019-04-16 2020-10-27 江苏恒瑞医药股份有限公司 酪氨酸激酶抑制剂联合长春碱类药物在制备预防或治疗肿瘤疾病的药物中的用途
WO2021037185A1 (fr) * 2019-08-30 2021-03-04 江苏恒瑞医药股份有限公司 Inhibiteur de tyrosine kinase ayant une faible teneur en impuretés
CN112279838B (zh) * 2020-10-29 2021-07-13 苏州富士莱医药股份有限公司 一种吡咯替尼的制备方法
CN114409584A (zh) * 2022-03-08 2022-04-29 重庆医药高等专科学校 一种1-甲基吡咯烷-2-甲醛的制备方法

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UA73073C2 (uk) * 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
KR100486394B1 (ko) * 1999-11-16 2005-04-29 쉬바르츠파르마에이지 3,3-디페닐-프로필아민의 신규한 유도체의 안정한 염
ATE370123T1 (de) * 2001-11-27 2007-09-15 Wyeth Corp 3-cyanochinoline als inhibitoren von egf-r- und her2-kinasen
DE10307165A1 (de) * 2003-02-20 2004-09-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, ihre Verwendung und Verfahren zu ihrer Herstellung
US7399865B2 (en) 2003-09-15 2008-07-15 Wyeth Protein tyrosine kinase enzyme inhibitors
CN100540552C (zh) * 2007-02-01 2009-09-16 中国药科大学 3-氰基喹啉衍生物、其制备方法及其医药用途
US8022216B2 (en) * 2007-10-17 2011-09-20 Wyeth Llc Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof
CN101824029A (zh) * 2009-03-05 2010-09-08 厦门艾德生物医药科技有限公司 酪氨酸激酶不可逆抑制剂、其药物组合物及其用途
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Also Published As

Publication number Publication date
US20130338190A1 (en) 2013-12-19
HK1177461A1 (en) 2013-08-23
KR20140009418A (ko) 2014-01-22
WO2012122865A2 (fr) 2012-09-20
EP2684877A2 (fr) 2014-01-15
TW201236684A (en) 2012-09-16
KR101871889B1 (ko) 2018-06-27
JP2014507448A (ja) 2014-03-27
EP2684877A4 (fr) 2014-08-06
PT2684877T (pt) 2017-01-18
WO2012122865A3 (fr) 2012-11-08
RU2583056C2 (ru) 2016-05-10
JP6192544B2 (ja) 2017-09-06
ES2605564T3 (es) 2017-03-15
PL2684877T3 (pl) 2017-05-31
EP2684877B1 (fr) 2016-10-19
CN102933574A (zh) 2013-02-13
CN102675287A (zh) 2012-09-19
RU2013143381A (ru) 2015-04-20
CN102933574B (zh) 2014-10-01

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